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Assay Detail

CHEMBL4056997

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant FGFR1 (unknown origin) using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA based spectrophotometric analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fibroblast growth factor receptor 1 (CHEMBL3650)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of 1H-indazol-3-amine derivatives as potent fibroblast growth factor receptor inhibitors.
Cui J, Peng X, Gao D, Dai Y, Ai J, Li Y.
Bioorg Med Chem Lett (2017) 27 : 3782 -3786
PubMed 28687204 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.73 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3348846 FEXAGRATINIB 2.0 1 8.92
CHEMBL4086560 1 8.43
CHEMBL4096740 1 8.25
CHEMBL4076610 1 8.21
CHEMBL4078715 1 7.98
CHEMBL4104460 1 7.89
CHEMBL4081153 1 7.85
CHEMBL4090974 1 7.68
CHEMBL4079317 1 7.45
CHEMBL4076490 1 7.31
CHEMBL4099060 1 7.00
CHEMBL4087200 1 6.83
CHEMBL4105046 1 6.66
CHEMBL4092994 1 -
CHEMBL4072232 1 -
CHEMBL4105407 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3348846 FEXAGRATINIB IC50 = 1.2 nM 8.92
CHEMBL4086560 IC50 = 3.7 nM 8.43
CHEMBL4096740 IC50 = 5.6 nM 8.25
CHEMBL4076610 IC50 = 6.2 nM 8.21
CHEMBL4078715 IC50 = 10.4 nM 7.98
CHEMBL4104460 IC50 = 13.0 nM 7.89
CHEMBL4081153 IC50 = 14.0 nM 7.85
CHEMBL4090974 IC50 = 21.1 nM 7.68
CHEMBL4079317 IC50 = 35.2 nM 7.45
CHEMBL4076490 IC50 = 49.0 nM 7.31
CHEMBL4099060 IC50 = 99.3 nM 7.00
CHEMBL4087200 IC50 = 147.6 nM 6.83
CHEMBL4105046 IC50 = 219.6 nM 6.66
CHEMBL4092994 IC50 > 1000.0 nM -
CHEMBL4072232 IC50 > 1000.0 nM -
CHEMBL4105407 IC50 < 4.1 nM -